EP0098577A2 - Médicaments pour le traitement des diarrhées occasionnées par des infections - Google Patents

Médicaments pour le traitement des diarrhées occasionnées par des infections Download PDF

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Publication number
EP0098577A2
EP0098577A2 EP83106536A EP83106536A EP0098577A2 EP 0098577 A2 EP0098577 A2 EP 0098577A2 EP 83106536 A EP83106536 A EP 83106536A EP 83106536 A EP83106536 A EP 83106536A EP 0098577 A2 EP0098577 A2 EP 0098577A2
Authority
EP
European Patent Office
Prior art keywords
compound
medicament according
formula
general formula
methyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP83106536A
Other languages
German (de)
English (en)
Inventor
Elmar Dr. Schrinner
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Hoechst AG
Original Assignee
Hoechst AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoechst AG filed Critical Hoechst AG
Publication of EP0098577A2 publication Critical patent/EP0098577A2/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals

Definitions

  • Antibacterial, but also astringent or detoxifying substances are usually used to treat infectious diarrhea. With such diarrhea, the intestinal flora is changed; it is populated with pathogenic germs. The most important therapeutic measure is to kill these pathogenic germs. In addition, acute forms of diarrhea can also be expected to cause invasive invasion of the pathogens into the circulation. These pathogens cannot be detected by the usual non-absorbable antidiarrheal drugs.
  • acridine derivatives trypaflavin and ethacridine lactate like the quinoline derivatives clioquinol and halquinol, have an amoebicidal and bacteriostatic effect and can therefore be used against infectious diarrhea.
  • compounds from the series of nalidixic acids, both quinolinone compounds and naphthyridine compounds have a broad spectrum of antibacterial activity.
  • the invention relates to medicaments for the treatment of infectious diarrhea, as defined in the claims.
  • the basic idea of the invention is to create a new medicament for the treatment of such diarrhea, which consists of a compound which is amoebicidal and bactericidal or bacteriostatic in the intestinal lumen, combined with another compound which is absorbed in the digestive tract and has a systemic antibacterial effect. It has been found that certain combinations of such compounds are not only compatible, but in certain mixing ratios a strong synergism against a large part of infectious gram-positive and gram-negative germs.
  • a and B is the lowest concentration of the compounds A and B, which in combination with the compound B and A shows an inhibitory effect. This value is divided by the MIC of compound A and B.
  • the FIC index obtained in this way provides information about the Interactions of two compounds in their antibacterial effects. FIC index numbers that are less than 1 express a synergistic effect. The results obtained with this method are summarized in the tables below.
  • the minimum inhibitory concentrations of the tested compounds in micrograms per milliliter are listed in the first two columns in the tables below. In some cases, different concentration units are given, eg nanograms [ng] or milligrams [mg] per milliliter. When a FIC index was not specified, this means that due to the U n capablekeit of a drug was to determine no limit.
  • the experiments have shown that a combination of ethacridine lactate with 5-ethyl-5,8-dihydro-8-oxofuran (3,2-b) - (1,8) -naphthyridine-7-carboxylic acid gave the smallest FIC indices and thus had the greatest synergistic effect on the majority of the germs tested.
  • Ethacridine lactate, K 81'1355 A, maize starch, part of the cellulose powder, sodium amylopectin glycolate and highly disperse silicon dioxide are mixed.
  • the mixture is compacted with a suitable tablet press or a roller mill.
  • the compressed products obtained are passed through a sieve and the resulting granules are mixed with the rest of the highly disperse silicon dioxide, the rest of the cellulose powder, the rest of the Na-amylopectin glycolate and the total proportion of talc and magnesium stearate.
  • the granules formed in this way are pressed into tablets or dragee cores with a final weight of 310 mg.
  • the coated cores can be lacquered or coated.
  • Film formers known to the person skilled in the art such as low-viscosity hydroxypropylmethyl cellulose (for example Methocel E 5 cps or Pharmacoat 606), are used to produce film tablets.
  • the films can be sprayed as a solution in organic solvents (e.g. mixture of methylene chloride and ethanol) or water.
  • organic solvents e.g. mixture of methylene chloride and ethanol
  • plasticizers and dyes are added to the top coats.
  • the total amount of lacquer dry substance is 10 mg per film-coated tablet.
  • coated tablet cores are covered with a tablet blanket known to the person skilled in the art.
  • Essential components of a suspension used for drug application are e.g.
  • Purified water is used as the solvent or suspending medium for the auxiliaries.
  • the ingredients (1) - (6) are mixed homogeneously and filled into size 1 hard gelatin capsules.
  • the components (1) - (5) are mixed homogeneously and filled into size 1 hard gelatin capsules.

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EP83106536A 1982-07-07 1983-07-05 Médicaments pour le traitement des diarrhées occasionnées par des infections Withdrawn EP0098577A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19823225367 DE3225367A1 (de) 1982-07-07 1982-07-07 Arzneimittel zur behandlung von infektioes bedingten diarrhoeen
DE3225367 1982-07-07

Publications (1)

Publication Number Publication Date
EP0098577A2 true EP0098577A2 (fr) 1984-01-18

Family

ID=6167841

Family Applications (1)

Application Number Title Priority Date Filing Date
EP83106536A Withdrawn EP0098577A2 (fr) 1982-07-07 1983-07-05 Médicaments pour le traitement des diarrhées occasionnées par des infections

Country Status (3)

Country Link
EP (1) EP0098577A2 (fr)
JP (1) JPS5942315A (fr)
DE (1) DE3225367A1 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0187315A3 (en) * 1985-01-05 1987-08-12 Bayer Ag Basic quinolonecarboxylic-acid preparations
WO1995031199A1 (fr) * 1994-05-11 1995-11-23 P.N. Gerolymatos S.A. Utilisation de clioquinol dans le traitement d'infections provoquees par helicobacter, y compris h. pylori et de maladies apparentees

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH0713798B2 (ja) * 1985-10-17 1995-02-15 晴彦 水谷 電子楽器
JPH079575B2 (ja) * 1986-01-16 1995-02-01 カシオ計算機株式会社 空気流応答型電子楽器
JP2724390B2 (ja) * 1986-07-07 1998-03-09 ヤマハ株式会社 電子管楽器
JPS642099A (en) * 1987-06-25 1989-01-06 Yamaha Corp Pitch bend controller for electronic wind instrument
JP2604431B2 (ja) * 1987-12-28 1997-04-30 カシオ計算機株式会社 電子管楽器
JPH0728460A (ja) * 1991-12-12 1995-01-31 Casio Comput Co Ltd 電子管楽器

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0187315A3 (en) * 1985-01-05 1987-08-12 Bayer Ag Basic quinolonecarboxylic-acid preparations
US4772605A (en) * 1985-01-05 1988-09-20 Bayer Aktiengesellschaft Basic formulations of quinolonecarboxylic acids
WO1995031199A1 (fr) * 1994-05-11 1995-11-23 P.N. Gerolymatos S.A. Utilisation de clioquinol dans le traitement d'infections provoquees par helicobacter, y compris h. pylori et de maladies apparentees

Also Published As

Publication number Publication date
JPS5942315A (ja) 1984-03-08
DE3225367A1 (de) 1984-01-12

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PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

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Withdrawal date: 19840309

RIN1 Information on inventor provided before grant (corrected)

Inventor name: SCHRINNER, ELMAR, DR.